Murizatoclax  (Synonyms: AMG 397)

Murizatoclax (AMG 397) is a potent, selective and orally active inhibitor of myeloid leukemia 1 (MCL-1) inhibitor, with a K_i of 15 pM. Murizatoclax competitive binds to the BH3-binding groove of MCL1 with pro-apoptotic BCL-2 family members. Murizatoclax can be used for the research of cancer^[1][2].

AMG 397 potently disrupts the interaction between MCL1 and BIM in OPM2 cells, induces clear increases in Caspase-3/7 activity within one hour^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Murizatoclax (25-50 mg/kg; p.o. once or twice weekly) exhibits significant tumor regressions in mice bearing OPM2 xenografts^[2].
Murizatoclax (10-60 mg/kg; p.o. twice weekly) achieves 47% MOLM-13 orthotopic tumor growth inhibition (TGI), 99% TGI and 75% regression at the dose of 10, 30 and 60 mg/kg, respectively^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

765.44

C₄₂H₅₇ClN₄O₅S

2245848-05-7

Solid

White to off-white

O=C(C(C=C1)=CC2=C1OC[C@]3(CCCC4=C3C=CC(Cl)=C4)CN2C[C@@]5([H])[C@](CC5)([H])[C@](CN6C[C@](CCCC7)([H])N7CC6)(OC)/C=C/C[C@H](C)[C@H]8C)NS8(=O)=O

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Wang H, et, al. Targeting MCL-1 in cancer: current status and perspectives. J Hematol Oncol. 2021 Apr 21;14(1):67.  [Content Brief]

  [2]. Caenepeel S, et al. Abstract 6218: discovery and preclinical evaluation of AMG 397, a potent, selective and orally bioavailable MCL1 inhibitor. Cancer Res. 2020;80(16 Supplement):6218.